[Translation] A single-center, randomized, open-label, four-period, completely repeated crossover design, fasting-administered bioequivalence study of olopatadine hydrochloride nasal spray in healthy subjects

1）本研究以山东京卫制药有限公司生产的盐酸奥洛他定鼻喷雾剂（规格：30.5g：201mg，240喷，每喷665μg）为受试制剂，以Amneal Pharmaceuticals LLC持证的盐酸奥洛他定鼻喷雾剂（商品名：OLOPATADINE HYDROCHLORIDE，规格：665μg/喷，30.5g/瓶，含240喷）为参比制剂，评价受试制剂和参比制剂在空腹条件下给药的生物等效性及药代动力学特征。 2）考察受试制剂和参比制剂在健康人体中的安全性。

[Translation]

1) This study used the olopatadine hydrochloride nasal spray (specification: 30.5g: 201mg, 240 sprays, 665μg per spray) produced by Shandong Jingwei Pharmaceutical Co., Ltd. as the test preparation, and the olopatadine hydrochloride nasal spray (trade name: OLOPATADINE HYDROCHLORIDE, specification: 665μg/spray, 30.5g/bottle, containing 240 sprays) certified by Amneal Pharmaceuticals LLC as the reference preparation to evaluate the bioequivalence and pharmacokinetic characteristics of the test preparation and the reference preparation under fasting conditions. 2) Investigate the safety of the test preparation and the reference preparation in healthy humans.

Start Date15 Feb 2025

Sponsor / Collaborator

Yingkerui (Hengqin) Pharmaceutical Research Institute Co., Ltd.

CTR20250136

/ Active, not recruitingNot Applicable

盐酸奥洛他定片在健康受试者中空腹生物等效性研究

[Translation] Fasting bioequivalence study of olopatadine hydrochloride tablets in healthy subjects

主要研究目的：研究空腹状态下单次口服受试制剂盐酸奥洛他定片（规格：5 mg，江苏万高药业股份有限公司生产）与参比制剂盐酸奥洛他定片（阿洛刻®，规格：5 mg，NIPRO PHARMA CORPORATION KAGAMIISHI PLANT 生产）在健康参与者体内的药代动力学，评价空腹状态下口服两种制剂的生物等效性。次要研究目的：评估受试制剂盐酸奥洛他定片（规格：5 mg）和参比制剂盐酸奥洛他定片（阿洛刻®，规格：5 mg）在健康参与者中的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetics of the test preparation Olopatadine Hydrochloride Tablets (Specification: 5 mg, produced by Jiangsu Wangao Pharmaceutical Co., Ltd.) and the reference preparation Olopatadine Hydrochloride Tablets (Aloko®, Specification: 5 mg, produced by NIPRO PHARMA CORPORATION KAGAMIISHI PLANT) in healthy participants after a single oral administration under fasting conditions, and to evaluate the bioequivalence of the two preparations when taken orally under fasting conditions. The secondary purpose of the study is to evaluate the safety of the test preparation Olopatadine Hydrochloride Tablets (Specification: 5 mg) and the reference preparation Olopatadine Hydrochloride Tablets (Aloko®, Specification: 5 mg) in healthy participants.

Start Date16 Jan 2025

Sponsor / Collaborator

Jiangsu Vanguard Pharmaceutical Co.,Ltd.

CTR20243907

/ CompletedNot Applicable

盐酸奥洛他定片在健康人体空腹/餐后状态下的生物等效性试验

[Translation] Bioequivalence study of olopatadine hydrochloride tablets in healthy volunteers under fasting and fed conditions

主要目的：本研究以郑州韩都药业集团有限公司持证的盐酸奥洛他定片为受试制剂，协和麒麟株式会社持证的盐酸奥洛他定片（商品名：Allelock）为参比制剂，进行空腹/餐后状态下人体生物等效性试验，次要目的：评价受试制剂和参比制剂在健康受试者体内的生物等效性。

[Translation]

Main purpose: This study used Olopatadine Hydrochloride Tablets certified by Zhengzhou Handu Pharmaceutical Group Co., Ltd. as the test preparation and Olopatadine Hydrochloride Tablets (trade name: Allelock) certified by Kyowa Kirin Co., Ltd. as the reference preparation to conduct a human bioequivalence test under fasting/fed conditions. Secondary purpose: To evaluate the bioequivalence of the test preparation and the reference preparation in healthy subjects.

Start Date14 Nov 2024

Sponsor / Collaborator

Zhengzhou Handu Pharmaceutical Co. Ltd.

100 Clinical Results associated with Olopatadine Hydrochloride

100 Translational Medicine associated with Olopatadine Hydrochloride

100 Patents (Medical) associated with Olopatadine Hydrochloride

749

Literatures (Medical) associated with Olopatadine Hydrochloride

01 Apr 2025·INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES

Association between congenital Zika syndrome and hospitalizations during early childhood: a nationwide cohort study

Article

Author: Teixeira, Maria Gloria ; Paixão, Enny S ; Barreto, Mauricio L ; Tedde, João Guilherme G ; Silva, Thiago Cerqueira ; Costa, Maria da Conceição ; Cardim, Luciana ; Brickley, Elizabeth B ; Rodrigues, Laura

OBJECTIVES:

Congenital Zika Syndrome (CZS) has been linked to a wide spectrum of abnormalities. However, differences in hospitalization patterns between children with and without CZS have not yet been investigated.

METHODS:

We compared rates of hospital admissions for all and specific diseases, proportions of admission causes, and total length of hospital stay (LOS) between children with CZS and those without the syndrome. Adjusted incidence rate ratios (aIRR) and aLOS were estimated using negative binomial regression.

RESULTS:

Compared to those without CZS, the aIRR for all-cause hospitalizations in the CZS group ranged from 3.77 (95%CI: 3.47-4.06) in the neonatal period to 7.76 (95%CI: 6.91-8.61) at ages 2-4 years. Similar trends were observed for specific causes of admissions. Most admissions in the CZS group related to congenital malformations, neurological, respiratory and infectious diseases. aLOS ranged from 16.0 days [95%CI: 13.2-19.5] to 19.9 days among CZS patients and 6.0 days [95%CI: 5.9-6.2] to 9.3 days [95%CI: 9.3-9.4] for patients without the syndrome.

CONCLUSION:

Children born with CZS face significantly higher rates of hospitalization and longer stays compared to those without the syndrome during early childhood.

16 Mar 2025·JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES

A validated rp-HPLC method for simultaneous determination of olopatadine hydrochloride and its related substances in eye drop

Author: Samrina Nasir, Sumaya ; Hasan, Md. Abid ; Azmi, Sajia ; Jahan Sultana, Nursad ; Helal, Naima

Olopatadine Hydrochloride, a H1-receptor antagonist, widely used for Allergic Conjunctivitis.A HPLC method was created and validated for the quantification of olopatadine hydrochloride and its related substances in eye formulation in accordance with ICH standardsThe separation of olopatadine hydrochloride was done by using a 4.6-mm 15-cm; 5 μm packing USP L7 column with a mobile phase made up of a mixer of phosphate buffer, pH 3.0: Acetonitrile (72:28) ratio at a flow rate of 1.0 mL/min and injection volume 30 μL.A photodiode array detector was used at a wavelength of 299 nm.The validation parameters including specificity, LOD/LOQ, linearity, accuracy, precision, robustness, and solution stability, were verified for performance of the method.The linearity ranges were 0.02-0.40, 0.0004-0.008 and 0.0001-0.002 mg/mL for olopatadine hydrochloride, olopatadine-related compound B and olopatadine carbaldehyde, resp.The % recovery was within the 80-120%.When the column temperature and flow rate were changed, the system suitability resolution was still within the acceptable range.The solutions were stable after 24 h at both room temperature and 5°C temperatureFor the anal. of olopatadine hydrochloride and its impurity in pharmaceutical finished eye dosage form, the confirmed HPLC method can be a workable anal. approach.

01 Feb 2025·SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

Implantation of impressive chromatographic and built-in UV spectrophotometry approaches for sustainable Estimation of olopatadine and mometasone in pharmaceuticals; eco-scale and BAGI applications

Article

Author: Emad F Abbas, Ahmed ; El-Masry, Amal A ; Elsabour, Samah A ; Salem, Yomna A

The development of analytical methods that adhere to the principles of sustainable green chemistry is essential in the modern scientific arena. This research presents two novel methods for the concurrent quantification of olopatadine (OLO) and mometasone (MOM), targeting sustainable green chemistry principles in their raw materials, dosage forms and combined nasal spray formulations. The first method is a rapid isocratic high-performance liquid chromatography (HPLC) that achieves excellent resolution within 4 min, with retention times of 2.37 ± 0.1 min for OLO and 4.05 ± 0.1 min for MOM. It features optimal sensitivity, with detection limits of 0.13 µg/mL for OLO and 0.03 µg/mL for MOM. It utilizes a cyano column with an isocratic mobile phase of acetonitrile and 0.1 M OPA (50: 50, v/v), making it accessible to standard laboratory equipment. The second method is UV-visible spectrophotometry, which includes first-order derivative measurement (D1) and ratio derivative spectra (RDS) methods. These spectroscopic approaches provide linear response range of 0.2-20.0 µg/mL for OLO and 4.0-40.0 µg/mL for MOM, respectively serving as cost-effective alternatives for labs with limited resources. Validation results show high accuracy (98-102 %) and precision (RSD < 2 %). Green assessments using Eco-Scale indicate scores of 86 for HPLC and 100 for spectrophotometry, while the "blueness" concept via BAGI demonstrates strong sustainability with scores of 87.5 and 90. These methods effectively quantify OLO and MOM in their raw materials, different formulations and combined nasal spray, providing a sustainable and reliable approach for pharmaceutical analysis. This work is the first green assessment for the determination of OLO and MOM in pure drug and in the pharmaceutical formulations using less hazard solvent and simple technique.

News (Medical) associated with Olopatadine Hydrochloride

12 Sep 2024

·www.inotekcorp.com

Effective Non-Prescription Pink Eye Drops for Nocturnal Lagophthalmos Management – Benefits, Usage, and User Testimonials

Nocturnal lagophthalmos is a condition characterized by the inability to fully close the eyelids during sleep. This can lead to various eye health issues, including dryness, irritation, and increased risk of infections. Individuals with nocturnal lagophthalmos may experience symptoms such as discomfort, redness, and excessive tearing upon waking up. The condition can result in compromised eye protection and lubrication, which are essential for maintaining optimal eye health. Research has shown that nocturnal lagophthalmos can be linked to certain medical conditions, such as Bell’s palsy, facial nerve damage, or anatomical abnormalities. It is important for individuals experiencing symptoms of nocturnal lagophthalmos to consult with an eye care professional for proper diagnosis and management. Furthermore, untreated nocturnal lagophthalmos can lead to more serious complications, including corneal abrasions, ulcers, or infections. Therefore, early detection and appropriate treatment are crucial in preventing potential long-term damage to the eyes. By understanding the nature of nocturnal lagophthalmos and its impact on eye health, individuals can take proactive steps to address the condition and protect their vision. For more information on nocturnal lagophthalmos, please visit the American Academy of Ophthalmology website. When it comes to managing nocturnal lagophthalmos, using non-prescription pink eye drops can be highly beneficial in alleviating symptoms and promoting eye health. These over-the-counter solutions are designed to provide relief from inflammation and irritation, which are common issues associated with nocturnal lagophthalmos. Here are some key reasons why incorporating non-prescription pink eye drops into your treatment regimen is essential: Relieves Dryness: Nocturnal lagophthalmos can lead to dry eyes due to inadequate moisture during sleep. Pink eye drops help lubricate the eyes, reducing dryness and discomfort. Reduces Inflammation: Inflammation is a common symptom of lagophthalmos, and non-prescription pink eye drops containing anti-inflammatory properties can help minimize redness and swelling. Promotes Comfort: By providing immediate relief from discomfort and irritation, pink eye drops can enhance overall comfort levels and support better sleep quality. Prevents Infections: Properly formulated non-prescription pink eye drops can help create a protective barrier against potential infections, safeguarding your eye health. It is essential to choose high-quality non-prescription pink eye drops that are specifically designed for treating nocturnal lagophthalmos. Look for products that are gentle on the eyes, free from harsh chemicals, and suitable for long-term use. “For individuals experiencing nocturnal lagophthalmos, incorporating non-prescription pink eye drops into their nightly routine can significantly improve eye comfort and reduce symptoms of dryness and inflammation.” $35.66 $65.17 $29.00 $64.80 Non-steroid eye drops are commonly used to address inflammation in the eyes, including conditions like nocturnal lagophthalmos. These eye drops work by targeting the underlying inflammatory processes that can worsen symptoms and impact eye health. When selecting non-steroid eye drops for managing inflammation associated with nocturnal lagophthalmos, it is essential to choose products that are specifically formulated for ocular use. These eye drops typically contain active ingredients such as ketotifen or olopatadine, which help alleviate inflammation and reduce discomfort. Studies have shown that non-steroid eye drops can effectively reduce inflammation in the eyes without the side effects commonly associated with steroid-based medications. These eye drops are usually safe for long-term use and can provide symptomatic relief for individuals with conditions like nocturnal lagophthalmos. It is important to follow the recommended usage instructions provided by the manufacturer or healthcare provider when using non-steroid eye drops. Generally, these eye drops are administered as one to two drops in the affected eye(s) a few times a day or as needed to manage symptoms. It is crucial to consult with an eye care professional before starting any new eye drop regimen, especially if you have underlying health conditions or are taking other medications. Your eye doctor can recommend the most suitable non-steroid eye drops for your specific needs and ensure they are safe and effective for managing inflammation associated with nocturnal lagophthalmos. Non-prescription antibiotic eye drops play a vital role in managing nocturnal lagophthalmos by helping to prevent and treat secondary infections that can occur due to the condition. Using these eye drops can aid in reducing the risk of complications and supporting overall eye health. Antibiotic eye drops are specifically designed to target and eliminate harmful bacteria that may enter the eyes during sleep when the eyelids do not fully close. By applying these drops before bedtime, individuals with nocturnal lagophthalmos can create a protective barrier against potential infections, such as conjunctivitis (pink eye) or keratitis. One of the key benefits of non-prescription antibiotic eye drops is their convenience and ease of use. They are readily available over the counter, allowing individuals to access them without a prescription. This accessibility makes it simpler for those with nocturnal lagophthalmos to incorporate the drops into their nightly eye care routine. Moreover, non-prescription antibiotic eye drops are generally well-tolerated and safe for regular use. They are formulated to be gentle on the eyes while effectively combating bacteria, helping to maintain ocular health and comfort. It is essential to follow the instructions provided with the eye drops to ensure proper application and maximize their effectiveness. In a recent survey conducted among individuals with nocturnal lagophthalmos, over 80% reported experiencing a reduction in eye irritation and redness after using non-prescription antibiotic eye drops regularly. This positive feedback highlights the beneficial effects of incorporating these drops into a comprehensive eye care regimen for managing the condition. It is recommended to consult with an eye care professional before starting any new eye drop regimen, including non-prescription antibiotic drops, to ensure they are suitable for individual needs and do not interact with any existing medications. By utilizing non-prescription antibiotic eye drops as part of a proactive eye care approach, individuals with nocturnal lagophthalmos can help safeguard their eye health and minimize the risk of infections. Non-steroid eye drops play a crucial role in managing the symptoms of nocturnal lagophthalmos. These eye drops aim to reduce inflammation and provide relief from discomfort associated with the condition. Here’s how non-steroid eye drops can help alleviate the symptoms of nocturnal lagophthalmos: Reduction of Inflammation: Non-steroid eye drops contain ingredients that help reduce inflammation in the eyes. By targeting the inflammatory response, these eye drops can help alleviate redness, swelling, and irritation caused by nocturnal lagophthalmos. Pain Relief: Non-steroid eye drops can provide pain relief for individuals experiencing discomfort due to nocturnal lagophthalmos. The soothing properties of these eye drops can help alleviate soreness and sensitivity in the eyes. Improved Eye Moisture: Nocturnal lagophthalmos can lead to dry eyes, making them prone to irritation and discomfort. Non-steroid eye drops can help improve eye moisture levels, keeping the eyes lubricated and reducing dryness. “Using non-steroid eye drops has significantly improved my comfort level during the night. I no longer wake up with dry, irritated eyes, thanks to the soothing effects of these eye drops.” – Sarah K., Nocturnal Lagophthalmos Patient Research has shown that non-steroid eye drops are effective in managing the symptoms of various eye conditions, including nocturnal lagophthalmos. These eye drops are gentle yet powerful in providing relief and reducing inflammation in the eyes. When selecting non-steroid eye drops for nocturnal lagophthalmos, it is essential to choose a formula that is gentle, preservative-free, and suitable for long-term use. Consult with your healthcare provider or eye care specialist to determine the best non-steroid eye drops for your specific needs. Many individuals suffering from nocturnal lagophthalmos have reported positive experiences with non-prescription pink eye drops in managing their condition. Here are some testimonials highlighting the effectiveness of these eye drops: “I have been using non-prescription pink eye drops for my nocturnal lagophthalmos for a few weeks now, and I have noticed a significant improvement in my eye health. The drops help keep my eyes moist throughout the night and reduce the discomfort I used to experience.” – John D. “I was skeptical about using non-prescription eye drops at first, but after trying them for my nocturnal lagophthalmos, I am impressed with the results. My eyes feel more comfortable, and I wake up with fewer dryness symptoms.” – Sarah L. These testimonials demonstrate that non-prescription pink eye drops can be a valuable tool in managing the symptoms of nocturnal lagophthalmos and improving overall eye health. If you are experiencing similar issues, consider incorporating these eye drops into your nightly routine. When choosing non-prescription eye drops to manage nocturnal lagophthalmos, it’s essential to consider several factors to ensure effective results. Here are some tips to help you select the right eye drops: Consultation with a healthcare professional: Before purchasing any non-prescription eye drops, consult with an eye care specialist or healthcare provider to get guidance on the best options for managing your condition. Ingredient suitability: Look for eye drops specifically designed for dry eyes and nighttime eye care. Ingredients such as hyaluronic acid, glycerin, and vitamin E can help lubricate and protect the eyes while you sleep. Packaging and formulation: Opt for eye drops that come in single-dose vials or preservative-free packaging to reduce the risk of contamination and ensure the freshness of the product. Effectiveness and user reviews: Research and read user reviews of the eye drops to gauge their effectiveness in managing nocturnal lagophthalmos. Look for positive feedback and testimonials from users who have found relief from their symptoms. Allergy considerations: If you have known allergies or sensitivities to certain ingredients, make sure to review the label of the eye drops and avoid products that may trigger an allergic reaction. By following these tips and making an informed decision when selecting non-prescription eye drops for managing nocturnal lagophthalmos, you can ensure that you are using a product that is safe, effective, and tailored to your specific needs.

01 Feb 2024

·www.biospace.com

Opthea Strengthens Team with Key Clinical and Regulatory Hires

Dr. Julie Clark, SVP Clinical Development; Dr. Fang Li, SVP Regulatory Affairs, to join February 1st Experienced executives bring extensive track record in products for retinal and ophthalmology diseases MELBOURNE, Australia, Feb. 01, 2024 (GLOBE NEWSWIRE) -- Opthea Limited (ASX:OPT; NASDAQ:OPT, “Opthea”), a clinical-stage biopharmaceutical company developing novel therapies to treat highly prevalent and progressive retinal diseases, today announced the appointment of Julie Clark, MD, MS, as Senior Vice President (SVP), Clinical Development, and Fang Li, Ph.D. RAC, as SVP, Regulatory Affairs, effective February 1, 2024. Dr. Clark and Dr. Li will report to Opthea Chief Executive Officer, Frederic Guerard, PharmD, MS, and will join the Opthea Executive Management Team. “It is my great pleasure to welcome two ophthalmology experts, Dr. Clark and Dr. Li, to the Company as we prepare for the next stage in our growth and work towards advancing the development of sozinibercept (OPT-302),” said Dr. Guerard. “Their past contributions to the development and registration of ophthalmology therapies such as IZERVAY™, BEOVU®, and EYLEA®, will be instrumental to the potential success of our lead program investigating sozinibercept, currently in two Phase 3 pivotal trials.” Dr. Clark shared, “I am thrilled to join Opthea as we prepare to complete patient enrollment in the pivotal Phase 3 clinical program for sozinibercept in the first half of 2024. The majority of my career has been dedicated to the clinical development of novel therapies for retinal diseases. Sozinibercept could be the first new drug for wet age-related macular degeneration (AMD) in more than 15 years, with the potential to deliver superior visual gains when administered in combination with standard of care therapy. I look forward to contributing to bringing this novel product candidate to patients with serious retinal disease.” Dr. Li commented, “As we work towards the potential release of topline results for our Phase 3 program in mid-2025, I am excited to apply my expertise to support the development and execution of our regulatory strategy and potential filings for sozinibercept in the U.S. and other markets. I look forward to the opportunity to bring Opthea’s innovative potential medicine through the regulatory process for the benefit of patients with retinal diseases.” Julie Clark, MD, MS With more than 15 years of experience in ophthalmology medical and clinical development, Dr. Clark brings expertise in both early and late-stage programs, regulatory submissions, and approvals. Her contributions include substantial support for the approval and launches of retinal therapies such as EYLEA®, JETREA® and BEOVU®. In Dr. Clark’s most recent position as Vice President Clinical Development at IVERIC bio, Inc., An Astellas Company, she oversaw the development program leading to the August 2023 U.S. Food and Drug Administration (FDA) approval of IZERVAY™, a complement inhibitor approved for the treatment of geographic atrophy secondary to age-related macular degeneration. Dr. Clark previously served as Chief Medical Officer at Adverum Biotechnologies Inc, where she played a crucial role in developing intravitreal delivered gene therapy for retinal diseases. Dr. Clark is a graduate of Wake Forest University and Wake Forest University School of Medicine in Winston-Salem, NC, U.S. Fang Li, PhD, RAC Dr. Li brings over 30 years of expertise in drug development and more than 20 years in regulatory affairs experience. Her experience spans various domains including small molecules, biologics, gene therapy, over-the-counter products, in-vitro diagnostic products and medical devices, with a specific focus on ophthalmology. She has held key roles at prominent ophthalmology companies such as Novartis AG, Alcon Inc., and Bausch + Lomb Corporation. Dr. Li's extensive background includes significant involvement in health authority interactions, U.S. FDA advisory committee meeting preparation and the establishment and leadership of regulatory teams. She has a proven track record of success in obtaining product approvals in the U.S. and other regions. Throughout her career, Dr. Li has played a pivotal role in leading numerous FDA drug approvals, specifically contributing to the approval of ophthalmology products like JETREA®, LOTEMAX® Ointment, SYSTANE® COMPLETE. She has also contributed to the development and registration of other ophthalmology drug products such as BEOVU®, PAZEO®, LOTEMAX® GEL, BESIVANCE®, and VYZULTA®. Fang holds a PhD in Medicinal Chemistry from China Pharmaceutical University, China. About Opthea Opthea Limited (ASX:OPT; NASDAQ:OPT, “Opthea”) is a biopharmaceutical company developing novel therapies to address the unmet need in the treatment of highly prevalent and progressive retinal diseases, including neovascular (wet) age-related macular degeneration (wet AMD). Opthea’s lead product candidate sozinibercept is being evaluated in two pivotal Phase 3 clinical trials (ShORe, NCT04757610, and COAST, NCT04757636) for use in combination with standard-of-care anti-VEGF-A monotherapies to improve overall efficacy and deliver superior vision gains compared to standard-of-care. To learn more, visit and follow us on X and LinkedIn. Inherent risks of Investment in Biotechnology Companies There are a number of inherent risks associated with the development of pharmaceutical products to a marketable stage. The lengthy clinical trial process is designed to assess the safety and efficacy of a drug prior to commercialization and a significant proportion of drugs fail one or both of these criteria. Other risks include uncertainty of patent protection and proprietary rights, whether patent applications and issued patents will offer adequate protection to enable product development, the obtaining of necessary drug regulatory authority approvals and difficulties caused by the rapid advancements in technology. Companies such as Opthea are dependent on the success of their research and development projects and on the ability to attract funding to support these activities. Investment in research and development projects cannot be assessed on the same fundamentals as trading and manufacturing enterprises. Therefore, investment in companies specializing in drug development must be regarded as highly speculative. Opthea strongly recommends that professional investment advice be sought prior to such investments. Forward-looking Statements This ASX announcement contains certain forward-looking statements, including within the meaning of the U.S. Private Securities Litigation Reform Act of 1995. The words “expect”, “believe,” “should”, “could”, “may”, “will”, “plan” and other similar expressions are intended to identify forward-looking statements. Forward-looking statements in this ASX announcement include statements regarding expectations on the outcomes of Opthea’s Phase 3 clinical trials of sozinibercept, the potential for sozinibercept as a combination therapy to be the first therapy to achieve superior visual outcomes over anti-VEGF-A monotherapy and improve vision outcomes for patients with wet AMD, the expected timing for completion of enrollment for the Phase 3 studies and topline data, the market opportunity for sozinibercept, and the future performance of Opthea. Forward-looking statements, opinions and estimates provided in this ASX announcement are based on assumptions and contingencies which are subject to change without notice, as are statements about market and industry trends, which are based on interpretations of current conditions. Forward-looking statements are provided as a general guide only and should not be relied upon as an indication or guarantee of future performance. They involve known and unknown risks and uncertainties and other factors, many of which are beyond the control of Opthea and its directors and management and may involve significant elements of subjective judgment and assumptions as to future events that may or may not be correct. These statements may be affected by a range of variables which could cause actual results or trends to differ materially, including but not limited to future capital requirements, the development, testing, production, marketing and sale of drug treatments, regulatory risk and potential loss of regulatory approvals, ongoing clinical studies to demonstrate sozinibercept safety, tolerability and therapeutic efficacy, additional analysis of data from Opthea’s Phase 3 clinical trials, timing of completion of Phase 3 clinical trial patient enrollment and clinical research organization and labor costs, intellectual property protections, and other factors that are of a general nature which may affect the future operating and financial performance of the Company including risk factors set forth in Opthea’s Annual Report on Form 20-F filed with the U.S. Securities and Exchange Commission (the “SEC”) on September 28, 2023 and other future filings with the SEC. Actual results, performance or achievement may vary materially from any projections and forward-looking statements and the assumptions on which those statements are based. Subject to any continuing obligations under applicable law or any relevant ASX listing rules, Opthea disclaims any obligation or undertaking to provide any updates or revisions to any forward-looking statements in this ASX announcement to reflect any change in expectations in relation to any forward-looking statements or any change in events, conditions or circumstances on which any such statement is based, except as otherwise required by applicable law. Authorized for release to ASX by Frederic Guerard, CEO Company & Media Enquiries: Rudi Michelson Monsoon Communications Tel: +61 (0) 3 9620 3333 Investor Enquiries PJ Kelleher LifeSci Advisors Email: pkelleher@lifesciadvisors.com Join our email database to receive program updates: Tel: +61 (0) 3 9826 0399 Email: info@opthea.com Web:

Phase 3Executive ChangeDrug Approval

09 Jan 2024

·synapse.patsnap.com

Deciphering H1 receptor antagonists and Keeping Up with Their Recent Developments

The H1 receptor, also known as the histamine H1 receptor, plays a crucial role in the human body. It is primarily found in smooth muscle cells, endothelial cells, and nerve cells. Activation of the H1 receptor by histamine leads to various physiological responses, including vasodilation, increased vascular permeability, bronchoconstriction, and stimulation of sensory nerve endings. These responses are involved in allergic reactions, inflammation, and immune responses. Antagonists of the H1 receptor, commonly known as antihistamines, are widely used to treat allergies, hay fever, and other conditions associated with excessive histamine release. Understanding the role of the H1 receptor is essential for developing effective treatments for allergic and inflammatory disorders. The analysis of the target H1 receptor reveals a competitive landscape with multiple companies actively developing drugs. GSK Plc, Sanofi, Pfizer Inc., Bayer AG, and Novartis AG are among the companies with the highest number of approved drugs or drugs in advanced stages of development. The indications with the most approved drugs include Common Cold, Rhinitis, Allergic, Urticaria, Pruritus, and Hypersensitivity. Small molecule drugs are the most rapidly progressing drug type, indicating intense competition in this area. China, the United States, and Japan are the countries with the highest number of approved drugs, with China showing significant progress in the development of drugs targeting the H1 receptor. Overall, the target H1 receptor presents opportunities for further research and development, particularly in indications with high unmet medical needs. How do they work?H1 receptor antagonists, also known as H1 blockers or antihistamines, are a class of drugs that block the action of histamine at the H1 receptor. Histamine is a chemical released by the body during an allergic reaction, causing symptoms such as itching, sneezing, runny nose, and watery eyes. H1 receptor antagonists work by binding to the H1 receptors on cells, preventing histamine from binding and exerting its effects. From a biomedical perspective, H1 receptor antagonists are commonly used to treat allergic conditions, such as hay fever (allergic rhinitis), hives (urticaria), and allergic conjunctivitis. They help alleviate symptoms by reducing the effects of histamine, thereby relieving itching, sneezing, and other allergic reactions. There are different generations of H1 receptor antagonists, each with varying degrees of sedative effects. First-generation antihistamines, such as diphenhydramine and chlorpheniramine, can cause drowsiness and are often used for their sedative properties in addition to their antihistamine effects. Second-generation antihistamines, such as cetirizine, loratadine, and fexofenadine, are less likely to cause sedation and are preferred for daytime use. In summary, H1 receptor antagonists are drugs that block the action of histamine at the H1 receptor, providing relief from allergic symptoms. They are commonly used in the treatment of various allergic conditions and come in different generations with varying sedative effects. List of H1 receptor AntagonistsThe currently marketed H1 receptor antagonists include: Olopatadine Hydrochloride/Mometasone Furoate MonohydrateChlorpheniramine Maleate/Codeine PhosphateDiphenhydramine Hydrochloride/Naproxen SodiumRecombinant interferon alfa-2b/LoratadineRupatadine FumarateAzelastine/mometasoneEbastine/Pseudoephedrine HydrochlorideAzelastine Hydrochloride/Fluticasone PropionateChlorpheniramine Maleate/Hydrocodone Bitartrate/Pseudoephedrine HydrochlorideAlcaftadineFor more information, please click on the image below. What are H1 receptor antagonists used for?H1 receptor antagonists are widely used to treat allergies, hay fever, and other conditions associated with excessive histamine release. For more information, please click on the image below to log in and search. How to obtain the latest development progress of H1 receptor antagonists?In the Synapse database, you can keep abreast of the latest research and development advances of H1 receptor antagonists anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

100 Deals associated with Olopatadine Hydrochloride

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KEGG	Wiki	ATC	Drug Bank
D01192	Olopatadine Hydrochloride	R01AC08 S01GX09	DB00768

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Rhinitis, Allergic, Seasonal	United States	Novartis Pharmaceuticals Corp.	15 Apr 2008
Allergic rhinoconjunctivitis	Japan	Novartis Pharma KK	26 Jul 2006
Seasonal allergic conjunctivitis	European Union	Novartis Europharm Ltd.	16 May 2002
Seasonal allergic conjunctivitis	Australia	Novartis Pharmaceuticals Australia Pty Ltd.	16 May 2002
Seasonal allergic conjunctivitis	Iceland	Novartis Europharm Ltd.	16 May 2002
Seasonal allergic conjunctivitis	Liechtenstein	Novartis Europharm Ltd.	16 May 2002
Seasonal allergic conjunctivitis	Norway	Novartis Europharm Ltd.	16 May 2002
Pruritus	Japan	Kyowa Kirin Co., Ltd.	22 Dec 2000
Rhinitis, Allergic	Japan	Kyowa Kirin Co., Ltd.	22 Dec 2000
Urticaria	Japan	Kyowa Kirin Co., Ltd.	22 Dec 2000
Conjunctivitis, Allergic	United States	Alcon Laboratories, Inc.	18 Dec 1996

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute conjunctivitis	Phase 3	-	Alcon Research Ltd.	01 Oct 2009
Rhinitis, Allergic, Perennial	Phase 3	United States	Alcon Research Ltd.	01 Dec 2006
Rhinoconjunctivitis	Phase 3	-	Alcon Research Ltd.	18 Apr 2006

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


APAO2019	Not Applicable	Vernal Keratoconjunctivitis	96	Olopatadine 0.1%	zactlabhuc(mzvnoccudn) = xylwyywkrt zhubofthay (nhtodmbpzz )	Positive	06 Mar 2019
				Sodium Cromoglycate 2%	zactlabhuc(mzvnoccudn) = bjdbzbsfiv zhubofthay (nhtodmbpzz )
AAAAI2019	Not Applicable	Rhinitis, Allergic, Seasonal	-	GSP301 (olopatadine 665μg/mometasone 25μg BID)	pyuaehzzgi(pcnndhxmmt) = gxridikbze vyjtwvbnbs (tezaxbonvk, -0.41 to -0.05)	-	01 Feb 2019
NCT00609128 (CTgov)	Not Applicable	Conjunctivitis, Allergic \| Lacerations	21	olopatadine	xqshohqvan(rrwrzcdscx) = ffwvyxwsyo fnqrdllasa (ecvkrcsali, ifsptbgqsm - gpiztyjlhm) View more	-	20 Sep 2018
AAAAI2018	Not Applicable	Ragweed Sensitivity	180	GSP301 BID	lrytexerlg(uwrogwgxwj) = GSP301 BID had a rapid onset of action of 10 minutes and provided significant improvements in ocular symptoms vs placebo bnlwpvhdrk (mtxigfstva )	Positive	01 Feb 2018
AAAAI2018	Not Applicable	Rhinitis, Allergic, Seasonal	-	GSP301 (olopatadine 665μg/mometasone 25μg BID)	qrhwflenmd(uwcbqlkzkq) = uldrmidwyg ngywtjswbf (vahsjanrgh, -0.35[-0.63 - -0.07])	-	01 Feb 2018
ARVO2015	Phase 3	-	448	Olopatadine 0.77%	jsddoxbdyr(ueagjqwugb) = mkbkcoukwl tpycvgzdsp (hjkbgwyeyn )	Positive	01 Jun 2015
				Olopatadine 0.1%	jsddoxbdyr(ueagjqwugb) = unnwhflowo tpycvgzdsp (hjkbgwyeyn )
NCT01697969 (CTgov)	Phase 4	Conjunctivitis, Allergic	17	Olopatadine hydrochloride (Left Eye)	uivjhauila(bsvlehawwr) = iiadewixfk loyftonrmh (ddhvxteojn, 0.85) View more	-	18 Aug 2014
				Olopatadine hydrochloride (Right Eye)	uivjhauila(bsvlehawwr) = fdbcvlahsi loyftonrmh (ddhvxteojn, 0.92) View more
NCT01743027 (CTgov)	Phase 3	Conjunctivitis, Allergic	902	AL-4943A ophthalmic solution (AL-4943A)	ozveabllwh(fptpqljevn) = mfhcjwudke qfgipkammj (dlnqdqraxs, 0.069) View more	-	11 Aug 2014
				Olopatadine hydrochloride ophthalmic solution, 0.2% (PATADAY)	ozveabllwh(fptpqljevn) = yehzegsbto qfgipkammj (dlnqdqraxs, 0.069) View more
NCT01698814 (CTgov)	Phase 3	Conjunctivitis, Allergic	518	AL-4943A Ophthalmic Solution (AL-4943A)	rttckzfora = dtutuvljxl syjpaobhjn (kjbqwohlbo, emglcpqrpe - gdcktgpakj) View more	-	28 Feb 2014
				AL-4943A Ophthalmic Solution (AL-4943A Vehicle)	rttckzfora = dmwddeidfj syjpaobhjn (kjbqwohlbo, rizwudkgog - mssdlxfcgr) View more
NCT01732757 (CTgov)	Phase 4	Acute conjunctivitis \| Conjunctivitis, Allergic	157	Alcaftadine 0.25% (Lastacaft®)	xmdrsfxqrb(jrumopbjvm) = eybgpsttbz yercgsojam (xsxdvqddcx, 0.582) View more	-	14 Jan 2014
				Olopatadine 0.2% (Pataday™)	xmdrsfxqrb(jrumopbjvm) = qtfdqgeoze yercgsojam (xsxdvqddcx, 0.752) View more

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